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PMC5446412
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study
Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study Abstract Summary Background DSM265 is a novel antimalarial that inhibits plasmodial dihydroorotate dehydrogenase, an enzyme essential for pyrimidine biosynthesis. We ...
PMC10618299
core_pubmed_pmc
The effect of renal impairment and obesity on anti-Xa peak and trough levels in patients receiving therapeutic doses of nadroparin: a comparison with control patients
The effect of renal impairment and obesity on anti-Xa peak and trough levels in patients receiving therapeutic doses of nadroparin: a comparison with control patients Abstract Purpose Anti-Xa peak level monitoring is recommended during LMWH treatment in renal impairment or obesity. The trough level has been proposed as...
PMC12403662
core_pubmed_pmc
Novel guanidine derivatives as mechanistic scaffolds for anticancer agents: synthesis, characterization, DNA-binding, and computational studies
Novel guanidine derivatives as mechanistic scaffolds for anticancer agents: synthesis, characterization, DNA-binding, and computational studies Abstract Cancer continues to be a major global health challenge, necessitating the ongoing development of novel small-molecule therapeutics that can selectively target DNA and ...
PMC12838059
core_pubmed_pmc
In Vitro and In Vivo Evaluation of Nitroxoline as an Effective Antimicrobial Alternative to Poultry Production
In Vitro and In Vivo Evaluation of Nitroxoline as an Effective Antimicrobial Alternative to Poultry Production Abstract Background: Antimicrobial resistance is a major global challenge that is exacerbated by extensive antibiotic use in livestock farming. Identifying effective alternatives to widely used human antibioti...
PMC4879474
core_pubmed_pmc
Systems Pharmacology Modeling of Prostate‐Specific Antigen in Patients With Prostate Cancer Treated With an Androgen Receptor Antagonist and Down‐Regulator
Systems Pharmacology Modeling of Prostate‐Specific Antigen in Patients With Prostate Cancer Treated With an Androgen Receptor Antagonist and Down‐Regulator Abstract Abstract First‐in‐human (FIH) studies with AZD3514, a selective androgen receptor (AR) down‐regulator, showed decreases of >30% in the prostate‐specific an...
PMC5040008
core_pubmed_pmc
Montelukast in the treatment of perennial allergic rhinitis in paediatric Japanese patients; an open-label clinical trial
Montelukast in the treatment of perennial allergic rhinitis in paediatric Japanese patients; an open-label clinical trial Abstract Abstract Background : This study was conducted to evaluate the safety and tolerability, and population pharmacokinetics (PPK) of montelukast as well as efficacy in the treatment of perennia...
PMC4983555
core_pubmed_pmc
Alcohol and Aldehyde Dehydrogenases Contribute to Sex-Related Differences in Clearance of Zolpidem in Rats
Alcohol and Aldehyde Dehydrogenases Contribute to Sex-Related Differences in Clearance of Zolpidem in Rats Abstract Abstract Objectives: The recommended zolpidem starting dose was lowered in females (5 mg vs. 10 mg) since side effects were more frequent and severe than those of males; the mechanism underlying sex diffe...
PMC3282608
core_pubmed_pmc
Correlation between radioactivity and chemotherapeutics of the 111 In-VNB-liposome in pharmacokinetics and biodistribution in rats
Correlation between radioactivity and chemotherapeutics of the 111 In-VNB-liposome in pharmacokinetics and biodistribution in rats Abstract Abstract Background The combination of a radioisotope with a chemotherapeutic agent in a liposomal carrier (ie, Indium-111-labeled polyethylene glycol pegylated liposomal vinorelbi...
PMC4335513
core_pubmed_pmc
Pharmacokinetic variability and exposures of fluconazole, anidulafungin, and caspofungin in intensive care unit patients: Data from multinational Defining Antibiotic Levels in Intensive care unit (DALI) patients Study
Pharmacokinetic variability and exposures of fluconazole, anidulafungin, and caspofungin in intensive care unit patients: Data from multinational Defining Antibiotic Levels in Intensive care unit (DALI) patients Study Abstract Introduction The objective of the study was to describe the pharmacokinetics (PK) of fluconaz...
PMC12539419
core_pubmed_pmc
Renal Function and Hemoglobin Independently Predict Levetiracetam Exposure in Epilepsy Patients: A Multifactorial Regression Study
Renal Function and Hemoglobin Independently Predict Levetiracetam Exposure in Epilepsy Patients: A Multifactorial Regression Study Abstract Abstract Purpose To investigate the key factors influencing the plasma concentration of levetiracetam (LEV) in patients with epilepsy and to establish a predictive model for LEV st...
PMC5306496
core_pubmed_pmc
Population pharmacokinetics of daptomycin in adult patients undergoing continuous renal replacement therapy
Population pharmacokinetics of daptomycin in adult patients undergoing continuous renal replacement therapy Abstract Aim The objective of this population pharmacokinetic (PK) analysis was to provide guidance for the dosing interval of daptomycin in patients undergoing continuous renal replacement therapy (CRRT). Method...
PMC5397561
core_pubmed_pmc
Investigating Transporter‐Mediated Drug‐Drug Interactions Using a Physiologically Based Pharmacokinetic Model of Rosuvastatin
Investigating Transporter‐Mediated Drug‐Drug Interactions Using a Physiologically Based Pharmacokinetic Model of Rosuvastatin Abstract Rosuvastatin is a frequently used probe in transporter‐mediated drug‐drug interaction (DDI) studies. This report describes the development of a physiologically based pharmacokinetic (PB...
PMC3771370
core_pubmed_pmc
A phase Ib combination study of RO4929097, a gamma-secretase inhibitor, and temsirolimus in patients with advanced solid tumors
A phase Ib combination study of RO4929097, a gamma-secretase inhibitor, and temsirolimus in patients with advanced solid tumors Abstract Summary Background To determine the recommended phase II dose (RP2D) and assess the safety, pharmacokinetics (PKs) and pharmacodynamics of RO4929097in combination with temsirolimus. M...
PMC8612936
core_pubmed_pmc
Safety, pharmacokinetics, and antimalarial activity of the novel plasmodium eukaryotic translation elongation factor 2 inhibitor M5717: a first-in-human, randomised, placebo-controlled, double-blind, single ascending dose study and volunteer infection study
Safety, pharmacokinetics, and antimalarial activity of the novel plasmodium eukaryotic translation elongation factor 2 inhibitor M5717: a first-in-human, randomised, placebo-controlled, double-blind, single ascending dose study and volunteer infection study Abstract Background M5717 is the first plasmodium translation ...
PMC5937563
core_pubmed_pmc
Synergistic Activity of Colistin/Fosfomycin Combination against Carbapenemase-Producing Klebsiella pneumoniae in an In Vitro Pharmacokinetic/Pharmacodynamic Model
Synergistic Activity of Colistin/Fosfomycin Combination against Carbapenemase-Producing Klebsiella pneumoniae in an In Vitro Pharmacokinetic/Pharmacodynamic Model Abstract Carbapenemase-producing Klebsiella pneumoniae is globally recognized as one of the greatest threats to public health, and combination therapy may be...
PMC9830135
core_pubmed_pmc
P soralea corylifolia L.: a comprehensive review of its botany, traditional uses, phytochemistry, pharmacology, toxicology, quality control and pharmacokinetics
P soralea corylifolia L.: a comprehensive review of its botany, traditional uses, phytochemistry, pharmacology, toxicology, quality control and pharmacokinetics Abstract Psoralea corylifolia L. (PCL), referred to as “Bu-gu-zhi” in Chinese, has great medicinal values since ancient times. PCL is the dried ripe fruit of P...
PMC6009590
core_pubmed_pmc
Fusion Inhibitory Lipopeptides Engineered for Prophylaxis of Nipah Virus in Primates
Fusion Inhibitory Lipopeptides Engineered for Prophylaxis of Nipah Virus in Primates Abstract Abstract Background The emerging zoonotic paramyxovirus Nipah virus (NiV) causes severe respiratory and neurological disease in humans, with high fatality rates. Nipah virus can be transmitted via person-to-person contact, pos...
PMC6698815
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Considerations for the Use of Monoclonal Antibodies in the Treatment of Bacterial Infections
Pharmacokinetic and Pharmacodynamic Considerations for the Use of Monoclonal Antibodies in the Treatment of Bacterial Infections Abstract Abstract Antibiotic-resistant bacterial pathogens are increasingly implicated in hospital- and community-acquired infections. Recent advances in monoclonal antibody (mAb) production ...
PMC11898568
core_pubmed_pmc
Pharmacokinetic Characteristics of Tolfenamic Acid in Freshwater Crocodiles ( Crocodylus siamensis )
Pharmacokinetic Characteristics of Tolfenamic Acid in Freshwater Crocodiles ( Crocodylus siamensis ) Abstract Simple Summary Reptile analgesia data for pain management are not well-documented, with an even greater gap in knowledge for freshwater crocodiles, where drug dosing is commonly inferred from doses reported for...
PMC9458804
core_pubmed_pmc
Pharmacokinetics and Biochemical Efficacy of an α 1 -Proteinase Inhibitor (Aralast NP) in α 1 -Antitrypsin Deficiency: a Cross-Product Retrospective Comparability Analysis
Pharmacokinetics and Biochemical Efficacy of an α 1 -Proteinase Inhibitor (Aralast NP) in α 1 -Antitrypsin Deficiency: a Cross-Product Retrospective Comparability Analysis Abstract Introduction Augmentation therapy with plasma-derived α 1 -proteinase inhibitor (A1PI) products is currently the only approved disease-spec...
PMC12413966
core_pubmed_pmc
Assessing the Potential of Generative Artificial Intelligence Models to Assist Experts in the Development of Pharmacokinetic Models
Assessing the Potential of Generative Artificial Intelligence Models to Assist Experts in the Development of Pharmacokinetic Models Abstract Abstract Purpose: This study explores the potential of generative AI models to aid experts in developing scripts for pharmacokinetic (PK) models, with a focus on constructing a tw...
PMC9008526
core_pubmed_pmc
A Free Open-Source Bayesian Vancomycin Dosing App for Adults: Design and Evaluation Study
A Free Open-Source Bayesian Vancomycin Dosing App for Adults: Design and Evaluation Study Abstract Abstract Background It has been suggested that Bayesian dosing apps can assist in the therapeutic drug monitoring of patients receiving vancomycin. Unfortunately, Bayesian dosing tools are often unaffordable to resource-l...
PMC9161616
core_pubmed_pmc
A first-in-human phase 1/2 study of FGF401 and combination of FGF401 with spartalizumab in patients with hepatocellular carcinoma or biomarker-selected solid tumors
A first-in-human phase 1/2 study of FGF401 and combination of FGF401 with spartalizumab in patients with hepatocellular carcinoma or biomarker-selected solid tumors Abstract Background Deregulation of FGF19-FGFR4 signaling is found in several cancers, including hepatocellular carcinoma (HCC), nominating it for therapeu...
PMC9088354
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling Approaches for Patients With SARS‐CoV‐2 Infection: A Case Study With Imatinib
Physiologically Based Pharmacokinetic Modeling Approaches for Patients With SARS‐CoV‐2 Infection: A Case Study With Imatinib Abstract Abstract Severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) infection, which causes coronavirus disease 2019 (COVID‐19), manifests as mild respiratory symptoms to severe respir...
PMC8537465
core_pubmed_pmc
Population Pharmacokinetic Modelling of the Complex Release Kinetics of Octreotide LAR: Defining Sub-Populations by Cluster Analysis
Population Pharmacokinetic Modelling of the Complex Release Kinetics of Octreotide LAR: Defining Sub-Populations by Cluster Analysis Abstract The aim of the study is to develop a population pharmacokinetic (PPK) model, of Octreotide long acting repeatable (LAR) formulation in healthy volunteers, which describes the hig...
PMC3993894
core_pubmed_pmc
Injection Route and TLR9 Agonist Addition Significantly Impact Heroin Vaccine Efficacy
Injection Route and TLR9 Agonist Addition Significantly Impact Heroin Vaccine Efficacy Abstract Abstract Active immunization is an effective means of blocking the pharmacodynamic effects of drugs and holds promise as a treatment for heroin addiction. Previously, we demonstrated the efficacy of our first-generation vacc...
PMC12433208
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Modeling of Enteric-Coated Aspirin Capsule and Tablet Formulations in Healthy Subjects
Population Pharmacokinetic and Pharmacodynamic Modeling of Enteric-Coated Aspirin Capsule and Tablet Formulations in Healthy Subjects Abstract Abstract Purpose This study aimed to develop a population pharmacokinetic-pharmacodynamic (PK-PD) model to predict the PKs of acetylsalicylic acid (ASA) and salicylic acid (SA),...
PMC8002563
core_pubmed_pmc
Update on TDM (Therapeutic Drug Monitoring) with Ustekinumab, Vedolizumab and Tofacitinib in Inflammatory Bowel Disease
Update on TDM (Therapeutic Drug Monitoring) with Ustekinumab, Vedolizumab and Tofacitinib in Inflammatory Bowel Disease Abstract The goal of therapeutic drug monitoring (TDM) is to optimize anti-TNF (tumor necrosis factor) biologic treatment in patients with inflammatory bowel disease (IBD). Although commercial assays ...
PMC11761891
core_pubmed_pmc
Pharmacodynamic Profiling of Amoxicillin: Targeting Multidrug-Resistant Gram-Positive Pathogens Staphylococcus aureus and Staphylococcus pseudintermedius in Canine Clinical Isolates †
Pharmacodynamic Profiling of Amoxicillin: Targeting Multidrug-Resistant Gram-Positive Pathogens Staphylococcus aureus and Staphylococcus pseudintermedius in Canine Clinical Isolates † Abstract The rising threat of antimicrobial resistance (AMR) is a global concern in both human and veterinary medicine, with multidrug-r...
PMC4005281
core_pubmed_pmc
Surface modified multifunctional nanomedicines for simultaneous imaging and therapy of cancer
Surface modified multifunctional nanomedicines for simultaneous imaging and therapy of cancer Abstract Introduction: To date, a growing number of advanced anticancer nanomedicines (e.g., Doxil ® , Lipoxal ® , DepoCyte ® ) have entered into different phases of clinical trials. However, most of these medicaments fail to ...
PMC4576091
core_pubmed_pmc
Pharmacokinetics of Antituberculosis Drugs in HIV-Positive and HIV-Negative Adults in Malawi
Pharmacokinetics of Antituberculosis Drugs in HIV-Positive and HIV-Negative Adults in Malawi Abstract Limited data address the impact of HIV coinfection on the pharmacokinetics (PK) of antituberculosis drugs in sub-Saharan Africa. A total of 47 Malawian adults underwent rich pharmacokinetic sampling at 0, 0.5, 1, 2, 3,...
PMC11611767
core_pubmed_pmc
Anti‐tissue factor antibody conjugated with monomethyl auristatin E or deruxtecan in pancreatic cancer models
Anti‐tissue factor antibody conjugated with monomethyl auristatin E or deruxtecan in pancreatic cancer models Abstract Abstract Antibody–drug conjugates (ADCs) have been recognized as a promising class of cancer therapeutics. Tissue factor (TF), an initiator of the blood coagulation pathway, has been investigated regar...
PMC10543286
core_pubmed_pmc
Identifying novel radioprotective drugs via salivary gland tissue chip screening
Identifying novel radioprotective drugs via salivary gland tissue chip screening Abstract Abstract During head and neck cancer treatment, off-target ionizing radiation damage to the salivary glands commonly causes a permanent loss of secretory function. Due to the resulting decrease in saliva production, patients have ...
PMC6555167
core_pubmed_pmc
The role of fosfomycin in osteoarticular infection
The role of fosfomycin in osteoarticular infection Abstract Abstract Osteoarticular infections include septic arthritis and osteomyelitis, with Gram-positive microorganisms isolated most frequently. In recent years, there has been an increase in the number of resistant strains in this type of infection, which complicat...
PMC4338662
core_pubmed_pmc
The Open Physiology workflow: modeling processes over physiology circuitboards of interoperable tissue units
The Open Physiology workflow: modeling processes over physiology circuitboards of interoperable tissue units Abstract Abstract A key challenge for the physiology modeling community is to enable the searching, objective comparison and, ultimately, re-use of models and associated data that are interoperable in terms of t...
PMC5947839
core_pubmed_pmc
Efficacy, safety, and pharmacokinetics of budesonide/formoterol fumarate delivered via metered dose inhaler using innovative co-suspension delivery technology in patients with moderate-to-severe COPD
Efficacy, safety, and pharmacokinetics of budesonide/formoterol fumarate delivered via metered dose inhaler using innovative co-suspension delivery technology in patients with moderate-to-severe COPD Abstract Abstract Purpose This study investigated the efficacy, safety, and pharmacokinetics of the inhaled corticostero...
PMC9028991
core_pubmed_pmc
Population Pharmacokinetic (Pop-PK) Analysis of Torsemide in Healthy Korean Males Considering CYP2C9 and OATP1B1 Genetic Polymorphisms
Population Pharmacokinetic (Pop-PK) Analysis of Torsemide in Healthy Korean Males Considering CYP2C9 and OATP1B1 Genetic Polymorphisms Abstract Abstract Torsemide is a diuretic drug used for several cardiovascular and chronic diseases. With regard to the clinical application of torsemide, studies on individualized phar...
PMC10895684
core_pubmed_pmc
Evaluation of the cardiac safety of parsaclisib, a selective PI3Kδ inhibitor, in patients with previously treated B‐cell malignancies: Results from the CITADEL ‐101 study
Evaluation of the cardiac safety of parsaclisib, a selective PI3Kδ inhibitor, in patients with previously treated B‐cell malignancies: Results from the CITADEL ‐101 study Abstract Abstract Parsaclisib, a potent and selective phosphatidylinositol 3 kinase δ inhibitor, has been investigated for the treatment of B‐cell ma...
PMC8097458
core_pubmed_pmc
Drug-Drug Interaction Study of Benznidazole and E1224 in Healthy Male Volunteers
Drug-Drug Interaction Study of Benznidazole and E1224 in Healthy Male Volunteers Abstract E1224 is a prodrug of ravuconazole (RVZ), an antifungal drug with promising anti- Trypanosoma cruzi activity, the causative organism of Chagas disease (CD). This study was designed to assess the pharmacokinetics (PK) and safety in...
PMC12570623
core_pubmed_pmc
Bayesian joint spatiotemporal modelling of primary infection and reinfection of HFMD at county level in Jiangsu, China, 2009–2023
Bayesian joint spatiotemporal modelling of primary infection and reinfection of HFMD at county level in Jiangsu, China, 2009–2023 Abstract Over the past decade, multiple outbreaks of hand, foot, and mouth disease (HFMD) have occurred in East Asia, especially in China. It is crucial to understand the distribution patter...
PMC9296747
core_pubmed_pmc
Practical considerations for navigating the regulatory landscape of non-clinical studies for clinical translation of radiopharmaceuticals
Practical considerations for navigating the regulatory landscape of non-clinical studies for clinical translation of radiopharmaceuticals Abstract Abstract Background The development of radiopharmaceuticals requires extensive evaluation before they can be applied in a diagnostic or therapeutic setting in Nuclear Medici...
PMC6430890
core_pubmed_pmc
Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses
Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses Abstract Abstract Background Nonsteroidal anti‐inflammatory drugs are administered in horses for several systemic diseases. Selective cyclooxygenase‐2 inhibitors are preferred because of lower risk of adverse effects. Sev...
PMC5768226
core_pubmed_pmc
A Pharmacokinetics, Efficacy, and Safety Study of Gadoterate Meglumine in Pediatric Subjects Aged Younger Than 2 Years
A Pharmacokinetics, Efficacy, and Safety Study of Gadoterate Meglumine in Pediatric Subjects Aged Younger Than 2 Years Abstract Abstract Objectives The primary objective of this study was to investigate the pharmacokinetic profile of gadoterate meglumine in pediatric patients younger than 2 years; the secondary objecti...
PMC3468400
core_pubmed_pmc
Pharmacokinetic profiles of artesunate following multiple intravenous doses of 2, 4, and 8 mg/kg in healthy volunteers: Phase 1b study
Pharmacokinetic profiles of artesunate following multiple intravenous doses of 2, 4, and 8 mg/kg in healthy volunteers: Phase 1b study Abstract Abstract Background Severe malaria results in over a million deaths every year, most of them in children aged less than five years and living in sub-Saharan Africa. Injectable ...
PMC7485140
core_pubmed_pmc
Population Analysis of Anidulafungin in Infants to Older Adults With Confirmed or Suspected Invasive Candidiasis
Population Analysis of Anidulafungin in Infants to Older Adults With Confirmed or Suspected Invasive Candidiasis Abstract In a pooled population analysis, we investigated the pharmacokinetics of i.v. anidulafungin in four studies across a full range of adult and pediatric ages in patients with confirmed, suspected, or ...
PMC10085944
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of Glepaglutide, a Long-Acting GLP-2 Analog, in Subjects with Renal Impairment
Pharmacokinetics, Safety, and Tolerability of Glepaglutide, a Long-Acting GLP-2 Analog, in Subjects with Renal Impairment Abstract Background Glepaglutide is a novel, ready-to-use, long-acting, glucagon-like peptide-2 (GLP-2) analog intended for the treatment of patients with short bowel syndrome (SBS). This study inve...
PMC7105635
core_pubmed_pmc
Both Pharmacokinetic Variability and Granuloma Heterogeneity Impact the Ability of the First-Line Antibiotics to Sterilize Tuberculosis Granulomas
Both Pharmacokinetic Variability and Granuloma Heterogeneity Impact the Ability of the First-Line Antibiotics to Sterilize Tuberculosis Granulomas Abstract Tuberculosis (TB) remains as one of the world's deadliest infectious diseases despite the use of standardized antibiotic therapies. Recommended therapy for drug-sus...
PMC8840371
core_pubmed_pmc
Pharmacokinetic Outcomes of the Interactions of Antiretroviral Agents with Food and Supplements: A Systematic Review and Meta-Analysis
Pharmacokinetic Outcomes of the Interactions of Antiretroviral Agents with Food and Supplements: A Systematic Review and Meta-Analysis Abstract Because pharmacokinetic changes in antiretroviral drugs (ARV), due to their concurrent administration with food or nutritional products, have become a clinical challenge, it is...
PMC10603860
core_pubmed_pmc
Time-Kill Analysis of Canine Skin Pathogens: A Comparison of Pradofloxacin and Marbofloxacin
Time-Kill Analysis of Canine Skin Pathogens: A Comparison of Pradofloxacin and Marbofloxacin Abstract Abstract Time-kill curves (TKCs) are more informative compared with the use of minimum inhibitory concentration (MIC) as they allow the capture of bacterial growth and the development of drug killing rates over time, w...
PMC9349574
core_pubmed_pmc
Comparative Pharmacokinetics of Tixagevimab/Cilgavimab (AZD7442) Administered Intravenously Versus Intramuscularly in Symptomatic SARS‐CoV‐2 Infection
Comparative Pharmacokinetics of Tixagevimab/Cilgavimab (AZD7442) Administered Intravenously Versus Intramuscularly in Symptomatic SARS‐CoV‐2 Infection Abstract Abstract AZD7442 (Evusheld) is a combination of two human anti‐severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) monoclonal antibodies (mAbs), tixage...
PMC11331923
core_pubmed_pmc
Phase I Study of Tivozanib Eye Drops in Healthy Volunteers and Patients with Neovascular Age-Related Macular Degeneration
Phase I Study of Tivozanib Eye Drops in Healthy Volunteers and Patients with Neovascular Age-Related Macular Degeneration Abstract Purpose To evaluate the safety, pharmacokinetics, and exploratory efficacy of tivozanib eye drops in healthy volunteers and patients with neovascular age-related macular degeneration (nAMD)...
PMC5090806
core_pubmed_pmc
Development of Antisense Drugs for Dyslipidemia
Development of Antisense Drugs for Dyslipidemia Abstract Abstract Abnormal elevation of low-density lipoprotein (LDL) and triglyceride-rich lipoproteins in plasma as well as dysfunction of anti-atherogenic high-density lipoprotein (HDL) have both been recognized as essential components of the pathogenesis of atheroscle...
PMC12421222
core_pubmed_pmc
A Phase I, Open-Label, Dose Escalation Study of Enoblituzumab in Children and Young Adults with B7-H3–Expressing Relapsed or Refractory Solid Tumors
A Phase I, Open-Label, Dose Escalation Study of Enoblituzumab in Children and Young Adults with B7-H3–Expressing Relapsed or Refractory Solid Tumors Abstract Abstract Purpose: This multicenter, phase I, cohort expansion study was performed to characterize the safety, pharmacokinetics, pharmacodynamics, immunogenicity, ...
PMC10005744
core_pubmed_pmc
Dissecting the Interactions between Chlorin e6 and Human Serum Albumin
Dissecting the Interactions between Chlorin e6 and Human Serum Albumin Abstract Chlorin e6 (Ce6) is among the most used sensitizers in photodynamic (PDT) and sonodynamic (SDT) therapy; its low solubility in water, however, hampers its clinical exploitation. Ce6 has a strong tendency to aggregate in physiological enviro...
PMC8841438
core_pubmed_pmc
Evaluation of the potential drug interactions mediated through P‐gp, OCT2, and MATE1/2K with filgotinib in healthy subjects
Evaluation of the potential drug interactions mediated through P‐gp, OCT2, and MATE1/2K with filgotinib in healthy subjects Abstract Abstract Filgotinib, a preferential Janus Kinase‐1 inhibitor, is approved in Europe and Japan for treatment of rheumatoid arthritis and is being developed for treatment of other chronic i...
PMC12363291
core_pubmed_pmc
Frontiers in hepatic drug delivery-grand challenges
Frontiers in hepatic drug delivery-grand challenges Methods Assessment of nanomaterials hepatic toxicity Different toxic effects on the liver and other organs have been associated with various nanomaterials, such as silica nanoparticles, metallic nanoparticles, or carbon nanotubes, among others. Most of the nanoparticl...
PMC9546347
core_pubmed_pmc
Effect of mild or moderate hepatic impairment on the pharmacokinetics of risdiplam
Effect of mild or moderate hepatic impairment on the pharmacokinetics of risdiplam Abstract Aim This phase I, multicentre, open‐label, nonrandomised, parallel‐group, two‐part study aimed to evaluate the effect of mild to moderate hepatic impairment on the pharmacokinetics (PK), safety and tolerability of a single oral ...
PMC5391385
core_pubmed_pmc
The effect of UGT1A9 , CYP2B6 and CYP2C9 genes polymorphism on individual differences in propofol pharmacokinetics among Polish patients undergoing general anaesthesia
The effect of UGT1A9 , CYP2B6 and CYP2C9 genes polymorphism on individual differences in propofol pharmacokinetics among Polish patients undergoing general anaesthesia Abstract Propofol (2,6-diisopropylphenol) is one of the safest and most commonly used anaesthetic agents for intravenous general anaesthesia. However, i...
PMC10046456
core_pubmed_pmc
Influence of Single-Nucleotide Polymorphisms on Clinical Outcomes of Capecitabine-Based Chemotherapy in Colorectal Cancer Patients: A Systematic Review
Influence of Single-Nucleotide Polymorphisms on Clinical Outcomes of Capecitabine-Based Chemotherapy in Colorectal Cancer Patients: A Systematic Review Abstract Simple Summary Colorectal cancer is one of the most prevalent neoplasms worldwide. Capecitabine is an oral fluoropyrimidine widely used to treat colorectal can...
PMC4951311
core_pubmed_pmc
A pharmacokinetic and safety study of a fixed oral dose of enzastaurin HCl in native Chinese patients with refractory solid tumors and lymphoma
A pharmacokinetic and safety study of a fixed oral dose of enzastaurin HCl in native Chinese patients with refractory solid tumors and lymphoma Abstract Purpose This study was conducted to assess the pharmacokinetics and safety of enzastaurin in native Chinese patients with refractory solid tumors and lymphoma. Methods...
PMC6590377
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Analyses for CPX‐351 in Patients With Hematologic Malignancies
Population Pharmacokinetics and Exposure‐Response Analyses for CPX‐351 in Patients With Hematologic Malignancies Abstract Abstract CPX‐351, a dual‐drug liposomal encapsulation of cytarabine and daunorubicin at a synergistic ratio, is approved in the United States for adults with newly diagnosed therapy‐related acute my...
PMC6527858
core_pubmed_pmc
FABP1 controls hepatic transport and biotransformation of Δ 9 -THC
FABP1 controls hepatic transport and biotransformation of Δ 9 -THC Abstract The increasing use of medical marijuana highlights the importance of developing a better understanding of cannabinoid metabolism. Phytocannabinoids, including ∆ 9 -tetrahydrocannabinol (THC), are metabolized and inactivated by cytochrome P450 e...
PMC9415544
core_pubmed_pmc
Implementation of Model-Based Dose Adjustment of Tobramycin in Adult Patients with Cystic Fibrosis
Implementation of Model-Based Dose Adjustment of Tobramycin in Adult Patients with Cystic Fibrosis Abstract Abstract Therapeutic drug monitoring (TDM) of tobramycin is widely performed in patients with cystic fibrosis (CF), but little is known about the value of model-informed precision dosing (MIPD) in this setting. W...
PMC8745304
core_pubmed_pmc
Radical Scavenging Activity and Pharmacokinetic Properties of Coumarin–Hydroxybenzohydrazide Hybrids
Radical Scavenging Activity and Pharmacokinetic Properties of Coumarin–Hydroxybenzohydrazide Hybrids Abstract Free radicals often interact with vital proteins, violating their structure and inhibiting their activity. In previous studies, synthesis, characterisation, and the antioxidative properties of the five differen...
PMC5171805
core_pubmed_pmc
Engineering the surface properties of a human monoclonal antibody prevents self-association and rapid clearance in vivo
Engineering the surface properties of a human monoclonal antibody prevents self-association and rapid clearance in vivo Abstract Abstract Uncontrolled self-association is a major challenge in the exploitation of proteins as therapeutics. Here we describe the development of a structural proteomics approach to identify t...
PMC7559794
core_pubmed_pmc
Levers to Improve Antibiotic Treatment of Lambs via Drinking Water in Sheep Fattening Houses: The Example of the Sulfadimethoxine/Trimethoprim Combination
Levers to Improve Antibiotic Treatment of Lambs via Drinking Water in Sheep Fattening Houses: The Example of the Sulfadimethoxine/Trimethoprim Combination Abstract Abstract To limit the spread of bacterial diseases in sheep fattening houses, antibiotics are often administered collectively. Collective treatments can be ...
PMC10961592
core_pubmed_pmc
Establishment of a pharmacokinetics and pharmacodynamics model of Schisandra lignans against hippocampal neurotransmitters in AD rats based on microdi-alysis liquid chromatography-mass spectrometry
Establishment of a pharmacokinetics and pharmacodynamics model of Schisandra lignans against hippocampal neurotransmitters in AD rats based on microdi-alysis liquid chromatography-mass spectrometry Abstract Abstract Objective: Our previous studies substantiated that the biological activity of Schisandra chinensis ligna...
PMC6033038
core_pubmed_pmc
Pharmacokinetics of metformin in patients with gastrointestinal intolerance
Pharmacokinetics of metformin in patients with gastrointestinal intolerance Abstract Aims To assess potential causes of metformin intolerance, including altered metformin uptake from the intestine, increased anaerobic glucose utilization and subsequent lactate production, altered serotonin uptake, and altered bile acid...
PMC8882081
core_pubmed_pmc
Prediction of drug–drug interaction potential mediated by transporters between dasatinib and metformin, pravastatin, and rosuvastatin using physiologically based pharmacokinetic modeling
Prediction of drug–drug interaction potential mediated by transporters between dasatinib and metformin, pravastatin, and rosuvastatin using physiologically based pharmacokinetic modeling Abstract Abstract Purpose Recent in vitro studies demonstrated that dasatinib inhibits organic cation transporter 2 (OCT2), multidrug...
PMC9110613
core_pubmed_pmc
Patient-specific dosimetry adapted to variable number of SPECT/CT time-points per cycle for 177 Lu-DOTATATE therapy
Patient-specific dosimetry adapted to variable number of SPECT/CT time-points per cycle for 177 Lu-DOTATATE therapy Abstract Abstract Background The number of SPECT/CT time-points is important for accurate patient dose estimation in peptide receptor radionuclide therapy. However, it may be limited by the patient’s heal...
PMC12368586
core_pubmed_pmc
Continuous infusion versus intermittent dosing of ceftazidime/avibactam in critically ill patients with Klebsiella pneumoniae OXA-48 or Pseudomonas aeruginosa infections: a single-center randomized open-label trial (ZAVICONT). Rationale and design
Continuous infusion versus intermittent dosing of ceftazidime/avibactam in critically ill patients with Klebsiella pneumoniae OXA-48 or Pseudomonas aeruginosa infections: a single-center randomized open-label trial (ZAVICONT). Rationale and design Abstract Objective Ceftazidime/avibactam (CZA) is an essential treatment...
PMC3305926
core_pubmed_pmc
Intravenous pharmacokinetics, oral bioavailability, dose proportionality and in situ permeability of anti-malarial lumefantrine in rats
Intravenous pharmacokinetics, oral bioavailability, dose proportionality and in situ permeability of anti-malarial lumefantrine in rats Abstract Background Despite the wide spread use of lumefantrine, there is no study reporting the detailed preclinical pharmacokinetics of lumefantrine. For the development of newer ant...
PMC7287733
core_pubmed_pmc
PET Imaging of [ 11 C]MPC-6827, a Microtubule-Based Radiotracer in Non-Human Primate Brains
PET Imaging of [ 11 C]MPC-6827, a Microtubule-Based Radiotracer in Non-Human Primate Brains Abstract Abstract Dysregulation of microtubules is commonly associated with several psychiatric and neurological disorders, including addiction and Alzheimer’s disease. Imaging of microtubules in vivo using positron emission tom...
PMC5599481
core_pubmed_pmc
Challenges in translational drug research in neuropathic and inflammatory pain: the prerequisites for a new paradigm
Challenges in translational drug research in neuropathic and inflammatory pain: the prerequisites for a new paradigm Abstract Aim Despite an improved understanding of the molecular mechanisms of nociception, existing analgesic drugs remain limited in terms of efficacy in chronic conditions, such as neuropathic pain. He...
PMC12296188
core_pubmed_pmc
Harnessing Plant-Based Nanoparticles for Targeted Therapy: A Green Approach to Cancer and Bacterial Infections
Harnessing Plant-Based Nanoparticles for Targeted Therapy: A Green Approach to Cancer and Bacterial Infections Abstract Abstract This study investigates the antioxidant, antimicrobial, and antitumor activities of Taraxacum officinale (Dandelion) and Artemisia annua (Sweet Wormwood) extracts, along with their role in th...
PMC7392152
core_pubmed_pmc
Existing highly accumulating lysosomotropic drugs with potential for repurposing to target COVID-19
Existing highly accumulating lysosomotropic drugs with potential for repurposing to target COVID-19 Abstract Highlights • Lysosomotropic drugs show moderate antiviral effects even on coronaviruses. • The antiviral activity is likely due to interference with endosomal pathway. • 530 existing drugs were analysed for lyso...
PMC11007962
core_pubmed_pmc
First-in-human study of GFH018, a small molecule inhibitor of transforming growth factor-β receptor I inhibitor, in patients with advanced solid tumors
First-in-human study of GFH018, a small molecule inhibitor of transforming growth factor-β receptor I inhibitor, in patients with advanced solid tumors Abstract Background Transforming growth factor-β (TGF-β) is a cytokine with multiple functions, including cell growth regulation, extracellular matrix production, angio...
PMC10892858
core_pubmed_pmc
Model-Informed Drug Development: In Silico Assessment of Drug Bioperformance following Oral and Percutaneous Administration
Model-Informed Drug Development: In Silico Assessment of Drug Bioperformance following Oral and Percutaneous Administration Abstract Abstract The pharmaceutical industry has faced significant changes in recent years, primarily influenced by regulatory standards, market competition, and the need to accelerate drug devel...
PMC5486465
core_pubmed_pmc
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers Abstract Background Tenapanor (RDX5791, AZD1722), a small molecule with minimal systemic availability, is an inhibitor of the sodium/hydrogen exchanger isoform 3 (NHE3). Tenapanor acts locally...
PMC6700254
core_pubmed_pmc
Pharmacokinetic study of thymol after intravenous injection and high‐dose inhalation in mouse model
Pharmacokinetic study of thymol after intravenous injection and high‐dose inhalation in mouse model Abstract Abstract Thymol is generally recognized as a safe substance by the FDA and has been widely used in the pharmaceutical, food, and cosmetic industries. Pharmacokinetic (PK) studies of thymol have been previously c...
PMC11664934
core_pubmed_pmc
Population pharmacokinetics modelling for clinical dose adjustment of carboplatin in dogs
Population pharmacokinetics modelling for clinical dose adjustment of carboplatin in dogs Abstract Background Carboplatin is a human chemotherapeutic agent which is frequently used in dogs for the management of solid tumors. In human patient, its dosage is adjusted carefully, based on the creatinine clearance computati...
PMC9818718
core_pubmed_pmc
Increasing Dosage of Leucovorin Results in Pharmacokinetic and Gene Expression Differences When Administered as Two-Hour Infusion or Bolus Injection to Patients with Colon Cancer
Increasing Dosage of Leucovorin Results in Pharmacokinetic and Gene Expression Differences When Administered as Two-Hour Infusion or Bolus Injection to Patients with Colon Cancer Abstract Simple Summary 5-fluorouracil (5-FU) is the drug used in almost all chemotherapy regimens for colorectal cancer. To potentiate the d...
PMC11286092
core_pubmed_pmc
Does sildenafil citrate affect the pharmacokinetics of metformin in rats? Screening of mechanism through analytical and molecular docking approach
Does sildenafil citrate affect the pharmacokinetics of metformin in rats? Screening of mechanism through analytical and molecular docking approach Abstract Abstract OBJECTIVE: In the present study, the effect of sildenafil on the pharmacokinetics of metformin was studied in experimental rats, and we also postulated the...
PMC3552819
core_pubmed_pmc
Pharmacokinetics of a single oral dose of vitamin D3 (70,000 IU) in pregnant and non-pregnant women
Pharmacokinetics of a single oral dose of vitamin D3 (70,000 IU) in pregnant and non-pregnant women Abstract Abstract Background Improvements in antenatal vitamin D status may have maternal-infant health benefits. To inform the design of prenatal vitamin D3 trials, we conducted a pharmacokinetic study of single-dose vi...
PMC9441320
core_pubmed_pmc
The Cytokine Release Syndrome and/or the Proinflammatory Cytokines as Underlying Mechanisms of Downregulation of Drug Metabolism and Drug Transport: A Systematic Review of the Clinical Pharmacokinetics of Victim Drugs of this Drug–Disease Interaction Under Different Clinical Conditions
The Cytokine Release Syndrome and/or the Proinflammatory Cytokines as Underlying Mechanisms of Downregulation of Drug Metabolism and Drug Transport: A Systematic Review of the Clinical Pharmacokinetics of Victim Drugs of this Drug–Disease Interaction Under Different Clinical Conditions Abstract Background and Objective...
PMC11615940
core_pubmed_pmc
DeepCt: Predicting Pharmacokinetic Concentration–Time Curves and Compartmental Models from Chemical Structure Using Deep Learning
DeepCt: Predicting Pharmacokinetic Concentration–Time Curves and Compartmental Models from Chemical Structure Using Deep Learning Abstract After initial triaging using in vitro absorption, distribution, metabolism, and excretion (ADME) assays, pharmacokinetic (PK) studies are the first application of promising drug can...
PMC4031137
core_pubmed_pmc
Novel Epigenetic Target Therapy for Prostate Cancer: A Preclinical Study
Novel Epigenetic Target Therapy for Prostate Cancer: A Preclinical Study Abstract Abstract Epigenetic events are critical contributors to the pathogenesis of cancer, and targeting epigenetic mechanisms represents a novel strategy in anticancer therapy. Classic demethylating agents, such as 5-Aza-2′-deoxycytidine (Decit...
PMC12378882
core_pubmed_pmc
Assessing Safety of the Transition to Generic Imatinib in Patients with Gastrointestinal Stromal Tumours
Assessing Safety of the Transition to Generic Imatinib in Patients with Gastrointestinal Stromal Tumours Abstract Abstract Introduction Following patent expiration of branded imatinib (Glivec®), all Dutch patients with gastrointestinal stromal tumours (GIST) switched from Glivec to generic forms. Following this switch,...
PMC9718091
core_pubmed_pmc
Chondrocytic and pharmacokinetic properties of Phlpp inhibitors
Chondrocytic and pharmacokinetic properties of Phlpp inhibitors Abstract Abstract Objective The pleckstrin homology domain leucine-rich repeat protein phosphatases (Phlpp1/2) were recently identified as potential therapeutic targets for cartilage regeneration in osteoarthritic joints. Phlpp inhibitors NSC 117079 and NS...
PMC3664180
core_pubmed_pmc
Bioequivalance and pharmacokinetic study of febuxostat in human plasma by using LC-MS/MS with liquid liquid extraction method
Bioequivalance and pharmacokinetic study of febuxostat in human plasma by using LC-MS/MS with liquid liquid extraction method Abstract A bioequivalence study was proved of generic Febuxostat 80 mg tablets (T) in healthy volunteers.For this purpose, Authors developed a simple, sensitive, selective, rapid, rugged and rep...
PMC6647865
core_pubmed_pmc
A phase 1 dose escalation and expansion study of Tarextumab (OMP-59R5) in patients with solid tumors
A phase 1 dose escalation and expansion study of Tarextumab (OMP-59R5) in patients with solid tumors Abstract Summary Purpose This Phase I trial evaluated the maximum tolerated dose, safety, pharmacokinetics, pharmacodynamics and preliminary efficacy of tarextumab (OMP-5948), a novel cross-reactive antibody which binds...
PMC9092835
core_pubmed_pmc
Diagnostic biomarker kinetics: how brain-derived biomarkers distribute through the human body, and how this affects their diagnostic significance: the case of S100B
Diagnostic biomarker kinetics: how brain-derived biomarkers distribute through the human body, and how this affects their diagnostic significance: the case of S100B Abstract Blood biomarkers of neurological diseases are often employed to rule out or confirm the presence of significant intracranial or cerebrovascular pa...
PMC10515550
core_pubmed_pmc
Treatment of Severe COVID-19 Infection With Remdesivir in Peritoneal Dialysis
Treatment of Severe COVID-19 Infection With Remdesivir in Peritoneal Dialysis Abstract End-stage kidney disease (ESKD) has been shown to be correlated with an increased risk of COVID-19 infection and mortality. Remdesivir is an effective non-EUA U.S. Food and Drug Administration (FDA)-approved antiviral agent for the t...
PMC10014063
core_pubmed_pmc
Quantitative systems pharmacology of the eye: Tools and data for ocular QSP
Quantitative systems pharmacology of the eye: Tools and data for ocular QSP Abstract Abstract Good eyesight belongs to the most‐valued attributes of health, and diseases of the eye are a significant healthcare burden. Case numbers are expected to further increase in the next decades due to an aging society. The develop...
PMC3984057
core_pubmed_pmc
Advancing personalized care in hemophilia A: ten years’ experience with an advanced category antihemophilic factor prepared using a plasma/albumin-free method
Advancing personalized care in hemophilia A: ten years’ experience with an advanced category antihemophilic factor prepared using a plasma/albumin-free method Abstract Detailed analysis of data from studies of recombinant antihemophilic factor produced using a plasma/albumin-free method (rAHF-PFM) in previously treated...
PMC9166498
core_pubmed_pmc
Simultaneous and enantiospecific quantification of primaquine and carboxyprimaquine in human plasma using liquid chromatography-tandem mass spectrometry
Simultaneous and enantiospecific quantification of primaquine and carboxyprimaquine in human plasma using liquid chromatography-tandem mass spectrometry Abstract Background The enantiomers of the 8-aminoquinoline anti-malarial primaquine have different pharmacological properties. Development of an analytical method for...
PMC12840724
core_pubmed_pmc
Investigating the Therapeutic Effects of Naringenin and Oleuropein on Prostate Cancer Cell Mat-LyLu via miR-155-5p: A Bioinformatics and Molecular Docking Analysis of KRAS and CDK2 Networks
Investigating the Therapeutic Effects of Naringenin and Oleuropein on Prostate Cancer Cell Mat-LyLu via miR-155-5p: A Bioinformatics and Molecular Docking Analysis of KRAS and CDK2 Networks Abstract Background: This study systematically investigates the therapeutic effects of naringenin (NAR) and oleuropein (OLE) on pr...
PMC7395220
core_pubmed_pmc
Structural stability of SARS-CoV-2 3CLpro and identification of quercetin as an inhibitor by experimental screening
Structural stability of SARS-CoV-2 3CLpro and identification of quercetin as an inhibitor by experimental screening Abstract Abstract The global health emergency generated by coronavirus disease 2019 (COVID-19) has prompted the search for preventive and therapeutic treatments for its pathogen, the severe acute respirat...
PMC7422765
core_pubmed_pmc
Ranibizumab Population Pharmacokinetics and Free VEGF Pharmacodynamics in Preterm Infants With Retinopathy of Prematurity in the RAINBOW Trial
Ranibizumab Population Pharmacokinetics and Free VEGF Pharmacodynamics in Preterm Infants With Retinopathy of Prematurity in the RAINBOW Trial Abstract Purpose To develop a population pharmacokinetic (PK) model for intravitreal ranibizumab in infants with retinopathy of prematurity (ROP) and assess plasma free vascular...
PMC2885086
core_pubmed_pmc
Bioadhesive Controlled Metronidazole Release Matrix Based on Chitosan and Xanthan Gum
Bioadhesive Controlled Metronidazole Release Matrix Based on Chitosan and Xanthan Gum Abstract Metronidazole, a common antibacterial drug, was incorporated into a hydrophilic polymer matrix composed of chitosan xanthan gum mixture. Hydrogel formation of this binary chitosan-xanthan gum combination was tested for its ab...